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Assay Detail

CHEMBL5140366

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antiviral activity against drug-resistant HIV-1 Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
Ling X, Hao QQ, Pannecouque C, Clercq E, Chen FE.
Eur J Med Chem (2022) 238 : 114512 -114512
PubMed 35679690 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 43 5.44 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223228 EFAVIRENZ 4.0 1 8.15
CHEMBL308954 ETRAVIRINE 4.0 1 7.79
CHEMBL129 ZIDOVUDINE 4.0 1 7.62
CHEMBL5187988 1 6.12
CHEMBL5174000 1 5.85
CHEMBL5180920 1 5.72
CHEMBL5205629 1 5.46
CHEMBL5197703 1 5.41
CHEMBL5186337 1 5.40
CHEMBL5188407 1 5.39
CHEMBL5173017 1 5.36
CHEMBL5174481 1 5.28
CHEMBL5190637 1 5.28
CHEMBL5183294 1 5.26
CHEMBL5195817 1 5.24
CHEMBL5203279 1 5.19
CHEMBL5190141 1 5.16
CHEMBL5201823 1 5.14
CHEMBL57 NEVIRAPINE 4.0 1 5.11
CHEMBL5201738 1 5.06
CHEMBL374286 1 5.04
CHEMBL5204500 1 5.00
CHEMBL5202355 1 5.00
CHEMBL5191672 1 4.99
CHEMBL5176289 1 4.94
CHEMBL5190744 1 4.90
CHEMBL5188648 1 4.38
CHEMBL5186285 1 4.29
CHEMBL5181568 1 4.29
CHEMBL5174260 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223228 EFAVIRENZ EC50 = 7.1 nM 8.15
CHEMBL308954 ETRAVIRINE EC50 = 16.2 nM 7.79
CHEMBL129 ZIDOVUDINE EC50 = 24.2 nM 7.62
CHEMBL5187988 EC50 = 750.0 nM 6.12
CHEMBL5174000 EC50 = 1400.0 nM 5.85
CHEMBL5180920 EC50 = 1910.0 nM 5.72
CHEMBL5205629 EC50 = 3470.0 nM 5.46
CHEMBL5197703 EC50 = 3920.0 nM 5.41
CHEMBL5186337 EC50 = 3990.0 nM 5.40
CHEMBL5188407 EC50 = 4110.0 nM 5.39
CHEMBL5173017 EC50 = 4410.0 nM 5.36
CHEMBL5190637 EC50 = 5280.0 nM 5.28
CHEMBL5174481 EC50 = 5230.0 nM 5.28
CHEMBL5183294 EC50 = 5520.0 nM 5.26
CHEMBL5195817 EC50 = 5820.0 nM 5.24
CHEMBL5203279 EC50 = 6430.0 nM 5.19
CHEMBL5190141 EC50 = 6890.0 nM 5.16
CHEMBL5201823 EC50 = 7270.0 nM 5.14
CHEMBL57 NEVIRAPINE EC50 = 7711.6 nM 5.11
CHEMBL5201738 EC50 = 8700.0 nM 5.06
CHEMBL374286 EC50 = 9210.0 nM 5.04
CHEMBL5204500 EC50 = 10100.0 nM 5.00
CHEMBL5202355 EC50 = 9980.0 nM 5.00
CHEMBL5191672 EC50 = 10160.0 nM 4.99
CHEMBL5176289 EC50 = 11400.0 nM 4.94
CHEMBL5190744 EC50 = 12540.0 nM 4.90
CHEMBL5188648 EC50 = 41300.0 nM 4.38
CHEMBL5186285 EC50 = 50700.0 nM 4.29
CHEMBL5181568 EC50 = 51200.0 nM 4.29
CHEMBL5194378 EC50 - -
CHEMBL5192943 EC50 > 12860.0 nM -
CHEMBL5170052 EC50 > 68100.0 nM -
CHEMBL5199869 EC50 > 37100.0 nM -
CHEMBL5180025 EC50 > 47080.0 nM -
CHEMBL5170094 EC50 > 41120.0 nM -
CHEMBL5183658 EC50 > 23140.0 nM -
CHEMBL5169873 EC50 = 185600.0 nM -
CHEMBL5208866 EC50 > 39790.0 nM -
CHEMBL5171797 EC50 > 164080.0 nM -
CHEMBL5171760 EC50 > 362770.0 nM -
CHEMBL5175287 EC50 > 60870.0 nM -
CHEMBL5193413 EC50 > 70220.0 nM -
CHEMBL5174260 EC50 > 113150.0 nM -